Targeting VEGF–neuropilin interactions: a promising antitumor strategy. Issue 2 (February 2019) - Peng, Kewen
Highlights: Neuropilins (NRP) have been identified as essential coreceptors for vascular endothelial growth factors (VEGF). VEGF-NRP interactions exert multifaceted effects on tumor biology. Structural basis and characteristics of VEGF-NRP interactions guide antagonist design. Various peptide-based and small molecular NRP antagonists are introduced in detail. Abstract : Inhibition of vascular endothelial growth factor (VEGF) or its corresponding receptor (VEGFR) has been validated as an efficacious antiangiogenetic approach for cancer treatment. More recently, neuropilins (NRPs), the essential coreceptors for VEGF, have also been shown to have a significant role in VEGF signaling. Given the multifaceted effects of VEGF–NRP interactions on tumor initiation and progression, the exploration of new chemical entities that selectively block these interactions has recently attracted considerable interest as a novel antitumor strategy. Here, we summarize the biological functions of VEGF–NRP interactions in tumor biology, analyze the structural basis for these interactions, and present a detailed discussion of the development of the NRP antagonists reported so far.